Chlorambucil (Chlorambucilum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
Read on
Clinical and pharmacological group: & nbsp

Alkylating agents

Included in the formulation
  • Leukeran®
    pills inwards 
    Aspen Pharma Trading Limited    
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    L.01.A.A.02   Chlorambucil

    Pharmacodynamics:

    In the nuclei of tumor cells produces an alkylating effect on DNA molecules, disconnecting the nucleotide chains. As a result, DNA synthesis in tumor cells ceases.

    Suppresses the synthesis of lymphocytes, to a lesser extent - neutrophils, platelets and erythrocytes.

    Pharmacokinetics:

    After oral administration, the empty stomach is completely absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved after 0.25-2 hours. The connection with plasma proteins is 99%.

    Metabolism in the liver to the active metabolite - phenylacetic mustard.

    Half-life is 1.5 hours; for the active metabolite - 2.5 hours. Elimination by the kidneys.

    Indications:

    It is used to treat lymphogranulomatosis, Hodgkin's disease, chronic lymphocytic leukemia, Waldenstrom's macroglobulinemia, breast cancer, inoperable ovarian adenocarcinoma, chorionepithelioma of the uterus, nephrotic syndrome.

    ICD-10

    II.C51-C58.C54.9   Malignant neoplasm of uterine body, unspecified

    II.C81-C96.C88.0   Waldenstrom's macroglobulinemia

    II.C81-C96.C96.0   Disease Letterter-Sieve (non-lipid reticuloendotheliosis, reticulosis)

    II.C50.C50   Malignant neoplasm of breast

    II.C51-C58.C56   Malignant neoplasm of ovary

    II.C51-C58.C58   Malignant neoplasm of placenta

    II.C81-C96.C81   Hodgkin's disease [lymphogranulomatosis]

    II.C81-C96.C82   Follicular [nodular] non-Hodgkin's lymphoma

    II.C81-C96.C83   Diffuse non-Hodgkin's lymphoma

    II.C81-C96.C84   Peripheral and cutaneous T-cell lymphomas

    II.C81-C96.C85   Other and unspecified types of non-Hodgkin's lymphoma

    II.C81-C96.C85.0   Lymphosarcoma

    II.C81-C96.C91.1   Chronic lymphocytic leukemia

    II.C81-C96.C91.4   Hairy cell leukemia (Leukemic reticuloendotheliosis)

    II.C81-C96.C92   Myeloid leukemia [myeloid leukemia]

    XIV.N00-N08.N04   Nephrotic syndrome

    Contraindications:

    Hepatic and renal failure, epilepsy, bone marrow hypoplasia, individual intolerance.

    Carefully:

    Previous (less than 4-6 weeks) radiation therapy, urolithiasis, chicken pox, shingles, gout, head trauma, hyperuricemia, hypersensitivity.

    Pregnancy and lactation:

    Recommendations for FDA - category D. Contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Inside, to 0,1-0,2 mg / kg of body weight. The treatment schedule is determined individually.

    Side effects:

    Central and peripheral nervous system: tremor, hallucinations, cerebral circulation disorders, peripheral neuropathy, convulsive seizures in children with nephrotic syndrome.

    Respiratory system: shortness of breath, cough, interstitial pneumonia and fibrosis.

    Hemopoietic system: anemia, leukopenia, thrombocytopenia, rarely - irreversible bone marrow aplasia.

    The cardiovascular system: edema, hemorrhage, bleeding.

    Digestive system: ulceration of the oral mucosa, jaundice, impaired liver function

    Musculoskeletal system: back pain, arthralgia, muscular tremor.

    Dermatological reactions: toxic epidermal necrosis, rash, erythema multiforme.

    Urinary system: aseptic cystitis, hematuria, hyperuricemia, dysuric disorders.

    Reproductive system: teratogenic effect, azoospermia, amenorrhea.

    Secondary malignancy, allergic reactions.

    Overdose:

    Ataxia, convulsive seizures, pancytopenia.

    Treatment is symptomatic, blood transfusion according to indications.

    Interaction:

    Reduces the effect of allopurinol, probenecid, colchicine, sulfinpyrazone.

    It lowers the convulsive threshold when used simultaneously with monoamine oxidase inhibitors, neuroleptics, tricyclic antidepressants.

    With simultaneous application with lovastatin, the risk of acute renal failure increases and necrosis of skeletal muscles.

    Increases toxicity phenylbutazone.

    Special instructions:

    Treatment is carried out under the control of a general blood test - before treatment and daily during the course of therapy.

    Myelosuppression caused by taking the drug, leads to the emergence of bacterial infections, reduces the regenerative processes of wound healing, promotes bleeding gums. It is recommended to sanitize the oral cavity before starting chemotherapy.

    In the treatment it is not recommended to drive vehicles and work with moving mechanisms.

    Instructions
    Up